Brown Scott M, Smith Cassandra E, Meuth Alex I, Khan Maloree, Aroor Annayya R, Cleeton Hannah M, Meininger Gerald A, Sowers James R, DeMarco Vincent G, Chandrasekar Bysani, Nistala Ravi, Bender Shawn B
Harry S. Truman Memorial Veterans Hospital, Columbia, Missouri 65201.
Department of Biomedical Sciences, University of Missouri, Columbia, Missouri 65211.
Endocrinology. 2017 Oct 1;158(10):3592-3604. doi: 10.1210/en.2017-00416.
Activation of the renin-angiotensin-aldosterone system is common in hypertension and obesity and contributes to cardiac diastolic dysfunction, a condition for which no treatment currently exists. In light of recent reports that antihyperglycemia incretin enhancing dipeptidyl peptidase (DPP)-4 inhibitors exert cardioprotective effects, we examined the hypothesis that DPP-4 inhibition with saxagliptin (Saxa) attenuates angiotensin II (Ang II)-induced cardiac diastolic dysfunction. Male C57BL/6J mice were infused with either Ang II (500 ng/kg/min) or vehicle for 3 weeks receiving either Saxa (10 mg/kg/d) or placebo during the final 2 weeks. Echocardiography revealed Ang II-induced diastolic dysfunction, evidenced by impaired septal wall motion and prolonged isovolumic relaxation, coincident with aortic stiffening. Ang II induced cardiac hypertrophy, coronary periarterial fibrosis, TRAF3-interacting protein 2 (TRAF3IP2)-dependent proinflammatory signaling [p-p65, p-c-Jun, interleukin (IL)-17, IL-18] associated with increased cardiac macrophage, but not T cell, gene expression. Flow cytometry revealed Ang II-induced increases of cardiac CD45+F4/80+CD11b+ and CD45+F4/80+CD11c+ macrophages and CD45+CD4+ lymphocytes. Treatment with Saxa reduced plasma DPP-4 activity and abrogated Ang II-induced cardiac diastolic dysfunction independent of aortic stiffening or blood pressure. Furthermore, Saxa attenuated Ang II-induced periarterial fibrosis and cardiac inflammation, but not hypertrophy or cardiac macrophage infiltration. Analysis of Saxa-induced changes in cardiac leukocytes revealed Saxa-dependent reduction of the Ang II-mediated increase of cardiac CD11c messenger RNA and increased cardiac CD8 gene expression and memory CD45+CD8+CD44+ lymphocytes. In summary, these results demonstrate that DPP-4 inhibition with Saxa prevents Ang II-induced cardiac diastolic dysfunction, fibrosis, and inflammation associated with unique shifts in CD11c-expressing leukocytes and CD8+ lymphocytes.
肾素-血管紧张素-醛固酮系统的激活在高血压和肥胖中很常见,并会导致心脏舒张功能障碍,而目前尚无针对该病症的治疗方法。鉴于最近有报告称抗高血糖肠促胰岛素增强型二肽基肽酶(DPP)-4抑制剂具有心脏保护作用,我们检验了以下假设:用沙格列汀(Saxa)抑制DPP-4可减轻血管紧张素II(Ang II)诱导的心脏舒张功能障碍。雄性C57BL/6J小鼠连续3周输注Ang II(500 ng/kg/分钟)或赋形剂,并在最后2周接受Saxa(10 mg/kg/天)或安慰剂。超声心动图显示Ang II诱导的舒张功能障碍,表现为室间隔壁运动受损和等容舒张期延长,同时伴有主动脉硬化。Ang II诱导心脏肥大、冠状动脉周围动脉纤维化、与心脏巨噬细胞(而非T细胞)基因表达增加相关的TRAF3相互作用蛋白2(TRAF3IP2)依赖性促炎信号传导[p-p65、p-c-Jun、白细胞介素(IL)-17、IL-18]。流式细胞术显示Ang II诱导心脏CD45+F4/80+CD11b+和CD45+F4/80+CD11c+巨噬细胞以及CD45+CD4+淋巴细胞增加。用Saxa治疗可降低血浆DPP-4活性,并消除Ang II诱导的心脏舒张功能障碍,且与主动脉硬化或血压无关。此外,Saxa减轻了Ang II诱导的动脉周围纤维化和心脏炎症,但未减轻心脏肥大或心脏巨噬细胞浸润。对Saxa诱导的心脏白细胞变化的分析显示,Saxa可使Ang II介导的心脏CD11c信使核糖核酸增加减少,并增加心脏CD8基因表达以及记忆性CD45+CD8+CD44+淋巴细胞。总之,这些结果表明,用Saxa抑制DPP-4可预防Ang II诱导的心脏舒张功能障碍、纤维化和炎症,这些变化与表达CD11c的白细胞和CD8+淋巴细胞的独特变化有关。